The present invention relates to a method for identifying a mycbp2 modulator.An appropriate modulator is modeled by the modulation of the mycbp2 ubiquitin E3 ligase activity through covalent modulation of either of the two catalytic cysteines (c4520 and c4572) or is dynamically presented, as well as the new C4520 is identified by hindering the movement of the mediator loop region present.The present invention also relates to the use of hydroxy group containing small molecules and peptides as proxy substrates for measuring mycbp2 ligase activity, and their use in methods of identifying modulators.
展开▼